1. Field of the Invention
The present invention relates to novel phytandiol amine derivatives and their use for treatment or prevention of acne. More particularly, the present invention relates to novel phytandiol amine derivatives and compositions for improving or alleviating acne comprising the above derivatives as active ingredient.
2. Description of the Related Art
Acne is inflammatory disease or disorder generally developed at sebum gland in hair follicle of skin, of which etiopathology, although unclear, is suggested as follows: Excess secretion of sebum triggered by testosterone, one of androgenic hormones, contributes to dyskeratinization of pilosebaceous canal, and in turn results in blockage in orifice for secretion of sebum, thereby accumulation of sebum in hair follicle. Excess accumulation of sebum is responsible for overgrowth of acne-causing bacteria, e.g. Propionibacterium acnes, in such follicle, and the lipase secreted from the bacteria hydrolyzes the accumulated sebum to form free fatty acids giving rise to inflammation through irritation of skin. Also, acne-causing bacteria, recognized as antigen, elicit immune reaction of individuals, resulting in inflammatory reaction. In accordance with such mechanism, papule and inflammatory acne are developed, and when aggravated, wall of the follicle is disrupted and sequentially tissues are injured, finally leading to lesions of vesicular and pustule.
In an effort to inhibit generation and development of acne, a variety of pharmaceuticals formulated in the form of oral-administered drug or external preparation have been developed and employed. Such pharmaceuticals are: (a) anti-androgen agent for regulating secretion of androgenic hormones; (b) non-steroidal antiphlogostic agent exhibiting antinflammtory function; and (c) antimicrobial agents such as resorcinol, benzoyl peroxide, erythromycin and tetracycline to inhibit a growth of acne-causing bacteria. Recently, it is commonly employed to treat acne using retinoic acid and vitamin A derivatives.
Most of therapeutics for acne, however, is unfortunately suffered from adverse effects including inhibition of growth of epiderm, irritation or dyskeratinization of skin, resistance to antimicrobial agents and applicability.
Therefore, the use of low-irritating antimicrobial extracted from several plants has been recently attempted for controlling acne-causing bacteria in the field of cosmetics. Unfortunately, recent attempts as above-mentioned have recognized some drawbacks: (a) low antimicrobial activity and (b) inefficiency of separation and purification of active ingredient from natural sources.
Under such circumstances, many researches have continuously focused on substances or compositions for treating acne disease or disorder with both better compatibility to human body and greater efficacy.
U.S. Pat. No. 6,168,798 discloses non-irritating compositions for treating acne and other skin conditions comprising salicylic acid as active ingredient, and U.S. Pat. No. 6,174,892 discloses a method of treating acne with 5-alpha reductase inhibitors such as finasteride.
In addition, U.S. Pat. No. 4,775,663 suggests compositions for treating acne containing benzofuran derivatives and U.S. Pat. No. 5,019,567 discloses benzoyl peroxide-quaternary ammonium lipophilic salicylate based pharmaceutical and cosmetic compositions and their use especially in treatment of acne.
Throughout this application, various patents are reference and citations are provided in parentheses. The disclosure of these patents in their entities are hereby incorporated by references into this application in order to more fully describe this invention and the state of the art to which this invention pertains.